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Cat. No.: HY-188006

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GSPT1 degrader-18

GSPT1 degrader-18 is a GSPT1 degrader that inhibits the proliferation of cancer cells. GSPT1 degrader-18 has weak ability to induce the formation of the GSPT1-CRBN/DDB1 ternary complex and belongs to a weak molecular glue. GSPT1 degrader-18 can be used in cancer-related research.

For research use only. We do not sell to patients.

CAS No.: 3052938-18-5
Formula: C₂₄H₂₂ClN₃O₄
Molecular Weight:451.90

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

GSPT1 degrader-18 Chemical Structure

CAS No.: 3052938-18-5

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- In Vitro
Chemical Information
Purity & Documentation
References
Calculators
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Biological Activity

Description

In Vitro

GSPT1 degrader-18 (Compound 4) exhibits moderate binding affinity to CRBN in TR-FRET competitive binding assays; it shows weak ability to induce the formation of the GSPT1-CRBN/DDB1 ternary complex, with the normalized ternary complex signal in AlphaLISA being less than 10%, and the pEC₅₀ detected by HTRF falling within the range of 5.5 to 6.5^[1].
GSPT1 degrader-18 exhibits potent antiproliferative activity against KG-1, Kelly, NCI-H929, and wild-type Hep3B cells (IC₅₀ ≤ 100 nM), while barely inhibiting the proliferation of GSPT1-mutated Hep3B G575N cells (IC₅₀ > 5 μM), confirming that its cytotoxicity depends on intact GSPT1 protein^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS No. 3052938-18-5
Molecular Weight 451.90
Formula C₂₄H₂₂ClN₃O₄
SMILES

O=C(NC1=CC=C(C)C(Cl)=C1)OCC2=CC3=C(C=C(C4C(NC(CC4)=O)=O)C(C)=N3)C=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Cottens S, et al. Gspt1 degrader compounds. WO2024167423A1, WIPO, 2024.

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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